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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2009-2-23
pubmed:abstractText
The present study aimed to investigate the effect of roxithromycin on the oral and intravenous pharmacokinetics of loratadine in rats. The pharmacokinetic parameters ofloratadine were measured after an orally (4 mg/kg) and intravenously (1 mg/kg) administration of loratadine in the presence or absence of roxithromycin (2.0 or 5.0 mg/kg). Compared with the control (given loratadine alone), the area under the plasma concentration-time curve (AUC) was significantly (2.0 mg/kg, P < 0.05; 5.0 mg/kg, P < 0.01) increased by (76.8-119.2)% in the presence of roxithromycin after oral administration of loratadine. The peak plasma concentration (Cmax) was significantly (2.0 mg/kg, P < 0.05; 5.0 mg/kg, P < 0.01) increased by (45.1-97.6)% in the presence of roxithromycin after oral administration of loratadine. Consequently, the relative bioavailability (R.B.) of loratadine was increased by 1.77- to 2.19-fold. In contrast, roxithromycin had no effect on any pharmacokinetic parameters of loratadine given intravenously. It suggested that roxithromycin may improve the oral bioavailability of loratadine by reducing first-pass metabolism of loratadine most likely mediated by P-glycoprotein (P-gp) and/or cytochrome P450 (CYP) 3A4 in the intestine and/or liver. In conclusion, the presence of roxithromycin significantly enhanced the bioavailability of loratadine in rats, it may be due to inhibition of both CYP 3A4-mediated metabolism and P-gp in the intestine and/or liver by the presence of roxithromycin.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0378-7966
pubmed:author
pubmed:issnType
Print
pubmed:volume
33
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
231-6
pubmed:dateRevised
2011-2-2
pubmed:meshHeading
pubmed:articleTitle
Effects of roxithromycin on the pharmacokinetics of loratadine after oral and intravenous administration of loratadine in rats.
pubmed:affiliation
College of Pharmacy, Yanbian University, Jilin, 133000, China.
pubmed:publicationType
Journal Article